Phenylindolylmethyldiaminopyrimidines (PIDAPs) as Potent Antimicrobials Against Staphylococcus Aureus

18 January 2021, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


We have ascertained that phenylindolylmethyldiaminopyrimidines (PIDAPs), stop the growth of USA300 MRSA at low micromolar concentrations. The controls, penicillin G and vancomycin, are able to stop the growth of MRSA at ~765 μM (256 μg/mL) and ~1.38 μM (2 μg/mL) respectively. We have also found out that PIDAPs are bactericidal at or close to the MIC. No activity was observed against Gram-negative pathogens. Other Gram-positive pathogens have not yet been tested. Based on a search through the ChEMBL database, PIDAPs are a novel class of chemicals with antimicrobial properties. A limited structure-function study suggests that the diaminopyrimidine is part of the pharmacophore. Unfortunately, we also detected potential dose-limiting toxicity on human cell lines. Further, detailed studies are needed.




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